The use of at least one nucleic acid based nuclear localization signal including a natural or synthetic m
3
G-CAP is shown to increase transmembrane transport of a molecular cargo, in particular large molecules, into the nucleus. The use of natural and synthetic m
3
G-CAP is disclosed and the effect shown with a natural RNA 5′ end nuclear localization signal composed of a 2,2,7-trimethylguanosine CAP (m
3
G-CAP) coupled to fluorescent Streptavidin in one example, and an antisense oligonucleotide in another. A methylenephosphonate modified m
3
G-CAP is shown to have improved stability in human serum and in cytosolic extract.
本发明展示了至少使用一个基于核酸的核定位信号,其中包括自然或合成的m3G-CAP,可增加分子货物的跨膜转运,尤其是大分子,进入细胞核。本发明揭示了自然和合成的m3G-CAP的使用,并且在一个示例中显示了一种由2,2,7-三甲基
鸟嘌呤CAP(m3G-CAP)组成的自然RNA 5'末端核定位信号与荧光
链霉亲和素偶联,以及在另一个示例中使用反义寡核苷酸。显示了甲基
磷酸酯修饰的m3G-CAP在人血清和胞质
提取物中具有改善的稳定性。